Vanderbilt University

Astra Lakemedel Aktiebolag

Tomas De Paulis

Robert M Kessler

Jeffrey A Clanton

Howard E Smith

Sven O Gren

Sten I Ramsby

Aaron Janowsky

David M Lovinger

Aaron Janowski

Michael H Ebert

William Hewlett

Peter Martin

Dennis E Schmidt

This invention describes the novel use of alkyl, alkoxyl, halogenyl, or hydroxy substituted dicinnamoylquinides as therapeutic agents for enhancing adenosine levels in the brain and peripheral organs. These agents are particularly useful in treating human diseases or conditions that benefit from acute or chronic elevated levels of adenosine, such as reperfusion injury, coronary or cerebral ischemia, coronary vasoconstriction, paroxysmal supraventricular tachycardia, hypertension, wound healing, diabetes, inflammation, or sleep disturbances. They can also be used to protect normal cells from chemotoxicity in patients undergoing cancer therapy, and reverse the behavioral effects of caffeine intake.

Substituted dicinnamoylquinides and their use in augmentation of adenonsine function

This invention provides compounds of the formula I ##STR1## wherein, R.sup.1, R.sup.2, and R.sup.3 are independently �a first halogen atom,! fluorine, chlorine, bromine, iodine, alkyl, alkenyl, alkynyl, alkoxy, alkenoxy, or alkynoxy, wherein R.sup.2 and R.sup.3 can also independently be H, wherein at least one of R.sup.1, R.sup.2, and R.sup.3 is �a second halogen atom! fluorine, bromine, iodine or is substituted with �a second halogen atom,! fluorine, bromine or iodine and R.sup.4 is H or lower alkyl. The invention also provides precursors of formula I, radioactive analogs of formula I, and methods of using the compounds for the identification of 5-HT-3 receptors and the detection and treatment of abnormal conditions associated therewith.

Substituted benzamides and radioligand analogs and methods of use

Novel, substituted benzamides in radioiodinated form are useful in radiopharmaceutical compositions in nuclear medicine as imaging agents to detect, visualize, and analyze the distribution and function of the dopamine D2 receptor in the mammalian brain. These compounds have a specific combination of lipophilicity and dopamine D2 receptor affinity required to attain a required image contrast. The iodinated benzamides identified by the above discovery can be made by reacting a trialkyltin substituted benzamide with an acid in the presence of radioactive iodine which, in turn, is generated by in situ oxidation of an appropriate iodide nuclide salt.

Radioiodinated benzamines and method of their use as radioimaging

Novel, substituted benzamides in radioiodinated form are useful in radiopharmaceutical compositions in nuclear medicine as imaging agents to detect, visualize, and analyze the distribution and function of the dopamine D-2 receptor in the mammalian brain. The substituted benzamides and their racemic mixtures or their optically resolved enantiomers can be made by reacting a trialyltin substituted benzamide with an acid in the presence of radioactive iodine, generated by in situ oxidation of an appropriate iodide nuclide salt.

Radioiodinated benzamines method of their use as radioimaging agents

Novel therapeutically active compounds of the formula ##STR1## wherein R is a straight or branched alkyl group with 6-18 carbon atoms, R.sup.1 is hydrogen, chlorine, bromine or an alkyl group with 1-3 carbon atoms and R.sup.2 is chlorine, bromine or an alkyl group with 1-3 carbon atoms; or a physiologically acceptable salt or an optical isomer thereof, methods and intermediates for their preparation, pharmaceutical preparations containing them and methods for their therapeutical use.

Benzamido-derivatives

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Nashville, TN, United States of America

Tomas De Paulis